1-.sup.11 C-D-Glucose and related compounds
    5.
    发明授权
    1-.sup.11 C-D-Glucose and related compounds 失效
    1-11C-D-葡萄糖及相关化合物

    公开(公告)号:US4439414A

    公开(公告)日:1984-03-27

    申请号:US342684

    申请日:1982-01-26

    IPC分类号: A61K51/00 A61K49/02

    CPC分类号: A61K51/00

    摘要: The novel compounds 1-.sup.11 C-D-glucose, 1-.sup.11 C-D-mannose, 1-.sup.11 C-D-galactose, 2-.sup.11 C-D-glucose, 2-.sup.11 C-D-mannose and 2-.sup.11 C-D-galactose which can be used in nuclear medicine to monitor the metabolism of glucose and galactose can be rapidly prepared by reaction of the appropriate aldose substrate with an alkali metal .sup.11 C-labeled cyanide followed by reduction with a Raney alloy in formic acid.

    摘要翻译: 新化合物1-11C-D-葡萄糖,1-11C-D-甘露糖,1-11C-D-半乳糖,2-11C-D-葡萄糖,2-11C-D-甘露糖和2-11C-D-半乳糖 可以用于核医学监测葡萄糖和半乳糖的代谢,可以通过合适的醛糖底物与碱金属11C标记的氰化物反应,然后用阮内合金在甲酸中还原,快速制备。

    Positron emitter labeled enzyme inhibitors
    6.
    发明授权
    Positron emitter labeled enzyme inhibitors 失效
    正电子发射体标记的酶抑制剂

    公开(公告)号:US4913891A

    公开(公告)日:1990-04-03

    申请号:US52921

    申请日:1987-05-22

    IPC分类号: A61K51/04

    CPC分类号: A61K51/0406 A61K2123/00

    摘要: This invention involves a new strategy for imaging and mapping enzyme activity in the living human and animal body using positron emitter-labeled suicide enzyme inactivators or inhibitors which become covalently bound to the enzyme as a result of enzymatic catalysis. Two such suicide inactivators for monoamine oxidase have been labeled with carbon-11 and used to map the enzyme subtypes in the living human and animal body using PET. By using positron emission tomography to image the distribution of radioactivity produced by the body penetrating radiation emitted by carbon-11, a map of functionally active monoamine oxidase activity is obtained. Clorgyline and L-deprenyl are suicide enzyme inhibitors and irreversibly inhibit monoamine oxidase. When these inhibitors are labeled with carbon-11 they provide selective probes for monoamine oxidase localization and reactivity in vivo using positron emission tomography.

    摘要翻译: 本发明涉及使用正电子发射体标记的自杀酶灭活剂或由于酶促催化而与酶共价结合的抑制剂在活的人和动物体中成像和测定酶活性的新策略。 已经用碳-11标记了两种用于单胺氧化酶的这种自杀灭活剂,并且用于使用PET对活的人和动物体中的酶亚型进行映射。 通过使用正电子发射断层扫描来对由碳-11发射的身体穿透辐射产生的放射性分布进行成像,获得功能活性单胺氧化酶活性的图谱。 Clorgyline和L-去肾上腺素是自杀性酶抑制剂,并且不可逆地抑制单胺氧化酶。 当这些抑制剂用碳-11标记时,它们使用正电子发射断层扫描为体内单胺氧化酶定位和反应性提供选择性探针。

    .sup.18 F-4-Fluoroantipyrine
    9.
    发明授权
    .sup.18 F-4-Fluoroantipyrine 失效
    18F-4-氟安替比林

    公开(公告)号:US4436717A

    公开(公告)日:1984-03-13

    申请号:US268422

    申请日:1981-05-29

    IPC分类号: A61K51/04 A61K43/00 A61K49/00

    CPC分类号: A61K51/0453 A61K2123/00

    摘要: The novel radioactive compound .sup.18 F-4-fluoroantipyrine having high specific activity which can be used in nuclear medicine in diagnostic applications, prepared by the direct fluorination of antipyrine in acetic acid with radioactive fluorine at room temperature and purifying said radioactive compound by means of gel chromatography with ethyl acetate as eluent is disclosed. The non-radioactive 4-fluoroantipyrine can also be prepared by the direct fluorination of antipyrine in acetic acid with molecular fluorine at room temperature and purified by means of gel chromotography with ethyl acetate eluent.

    摘要翻译: 在诊断应用中可用于核医学中的具有高比活性的新型放射性化合物18F-4-氟替平吡啶,其通过在室温下用放射性氟在乙酸中直接氟化安替比林并通过凝胶色谱法纯化所述放射性化合物 公开了乙酸乙酯作为洗脱剂。 非放射性4-氟替苯胺也可以通过在室温下用分配氟在乙酸中直接氟化安替比林并通过乙酸乙酯洗脱液的凝胶色谱法纯化来制备。

    No-carrier-added (NCA) aryl (18E) fluorides via the nucleophilic
aromatic substitution of electron rich aromatic rings
    10.
    发明授权
    No-carrier-added (NCA) aryl (18E) fluorides via the nucleophilic aromatic substitution of electron rich aromatic rings 失效
    无载体添加(NCA)芳基(18E)氟化物通过富含芳族芳环的亲核芳烃取代

    公开(公告)号:US5254726A

    公开(公告)日:1993-10-19

    申请号:US711684

    申请日:1991-06-07

    摘要: A method for synthesizing no-carrier-added (NCA) aryl [.sup.18 F] fluoride substituted aromatic aldehyde compositions bearing an electron donating group is described. The method of the present invention includes the step of reacting aromatic nitro aldehydes having a suitably protected hydroxyl substitutent on an electron rich ring. The reaction isThe U.S. Government has rights in this invention pursuant to Contract Number DE-AC02-76CH00016, between the U.S. Department of Energy and Associated Universities Inc.

    摘要翻译: 描述了一种合成具有给电子基团的无载体添加(NCA)芳基[18 F]氟取代的芳族醛组合物的方法。 本发明的方法包括使具有适当保护的羟基取代基的芳族硝基醛与富电子环反应的步骤。 该反应通过亲核芳族取代通过无载体添加(NCA)[18F]氟离子进行。 本发明的方法可用于合成各种无载体添加的芳基[18 F]氟化物组合物,包括6- [18 F]氟-L-多巴,2- [18 F]氟酪氨酸,6- [18 F]氟去甲肾上腺素, 和6- [18F]氟代多巴胺。 在通过本发明产生对映异构体的外消旋混合物的情况下,例如在6- [18 F]氟去甲肾上腺素的合成中,优选的方法还包括在手性HPLC柱上拆分外消旋混合物。 该方法导致高产率的对映体纯的[18 F]标记的异构体,例如[ - ] - 6- [18 F]氟去甲肾上腺素和[+] - 6- [18F]氟去甲肾上腺素。